Structure-based design of novel, dipeptide ligands targeting the pp60(Src) SH2 domain

被引:8
|
作者
Shahripour, A
Para, KS
Plummer, MS
Lunney, EA
Holland, DR
Rubin, JR
Humblet, C
Fergus, JH
Marks, JS
Saltiel, AR
Sawyer, TK
机构
[1] WARNER LAMBERT PARKE DAVIS, PARKE DAVIS PHARMACEUT RES, DEPT BIOCHEM, ANN ARBOR, MI 48105 USA
[2] WARNER LAMBERT PARKE DAVIS, PARKE DAVIS PHARMACEUT RES, DEPT SIGNAL TRANSDUCT, ANN ARBOR, MI 48105 USA
关键词
D O I
10.1016/S0960-894X(97)00190-X
中图分类号
R914 [药物化学];
学科分类号
100701 ;
摘要
Based on the X-ray structures of the pp60(Src) (Src) SH2 domain complexed with two high affinity phosphopeptide ligands (Glu-Pro-Gln-pTyr-Glu-Glu-Ile-Pro-Ile-Tyr-Leu, and Ac-pTyr-Glu-(D) under bar-Hcy-NH2; Hcy = homocyclohexylalanine), we report herein the design and structure-activity relationships of a series of novel dipeptide ligands targeting the Src SH2 domain. (C) 1997 Elsevier Science Ltd.
引用
收藏
页码:1107 / 1112
页数:6
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